Drug

D0013 | Bezafibrate

Molecular Formula C19H20ClNO4
Molecular Weight 361.8
Structure
State solid
Protein binding 94-96% of bezafibrate is bound to protein in human serum.
Half life 1-2 hours
Absorption Bezafibrate is almost completely absorbed after oral administration. The relative bioavailability of bezafibrate retard compared to the standard form is about 70%.
Trade names Bezalip
Description Antilipemic agent

C

C10AB02 Bezafibrate


[C10AB] Fibrates


[C10A] LIPID MODIFYING AGENTS, PLAIN


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system


Toxicity Dose Time Species Model Method Action Positive criterion Reference
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex I activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex IV activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex V activity Negative p < 0.05 3

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase 50 μM bovine heart mitochondria Measurement of complex I activity Negative p < 0.05 3
Succinate dehydrogenase 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
Quinol--cytochrome-c reductase 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
Cytochrome c oxidase 50 μM bovine heart mitochondria Measurement of complex IV activity Negative p < 0.05 3
ATP synthase 50 μM bovine heart mitochondria Measurement of complex V activity Negative p < 0.05 3

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 105 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H302 (50.48%): Harmful if swallowed [Warning Acute toxicity, oral]


H361 (59.05%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


P201, P202, P264, P270, P281, P301+P312, P308+P313, P330, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Warning

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.


H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]


H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


P201, P202, P264, P270, P281, P301+P312, P308+P313, P330, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
mouse LD50 intraperitoneal 500mg/kg (500mg/kg) Medicamentos de Actualidad. Vol. 15, Pg. 215, 1979.
man TDLo oral 1326mg/kg/37W (1326mg/kg) kidney, ureter, and bladder: "changes in tubules (including acute renal failure, acute tubular necrosis)" Lancet. Vol. 341, Pg. 371, 1993.
rat LD50 intraperitoneal 505mg/kg (505mg/kg) Medicamentos de Actualidad. Vol. 15, Pg. 215, 1979.
women TDLo oral 12mg/kg/18D-I (12mg/kg) American Journal of Gastroenterology. Vol. 94, Pg. 3626, 1999.
rat LD50 subcutaneous 1580mg/kg (1580mg/kg) Kiso to Rinsho. Clinical Report. Vol. 22, Pg. 4293, 1988.
rat LD50 oral 1082mg/kg (1082mg/kg) Kiso to Rinsho. Clinical Report. Vol. 22, Pg. 4293, 1988.
mouse LD50 subcutaneous 1635mg/kg (1635mg/kg) Drugs in Japan Vol. -, Pg. 1226, 1995.
mouse LD50 oral 723mg/kg (723mg/kg) Kiso to Rinsho. Clinical Report. Vol. 22, Pg. 4293, 1988.
monkey LDLo oral 2gm/kg (2000mg/kg) Kiso to Rinsho. Clinical Report. Vol. 22, Pg. 4337, 1988.
man TDLo oral 514mg/kg/60D- (514mg/kg) peripheral nerve and sensation: sensory change involving peripheral nerve British Medical Journal. Vol. 309, Pg. 929, 1994.

  • Arteriosclerosis

  • Arteriosclerosis coronary artery

  • Combined hyperlipidaemia

  • Coronary artery disease

  • Dyslipidaemia

  • Hypercholesterolaemia

  • Hyperlipidaemia

  • Hypertriglyceridaemia

  • Infarction

  • Pancreatitis

  • Renal failure

  • Type IV hyperlipidaemia

  • Anaemia (0.011)

  • Pruritus (0.034)

  • Abdominal pain

  • Alanine aminotransferase increased

  • Aspartate aminotransferase increased

  • Blood creatine phosphokinase increased

  • Bronchitis

  • Dermatitis

  • Diarrhoea

  • Dyspepsia

  • Gastritis

  • Gastrointestinal pain

  • Headache

  • Influenza

  • Pharyngitis

  • Rash

  • Tenosynovitis

  • 2-(4-(2-((4-CHLOROBENZOYL)AMINO)ETHYL)PHENOXY)-2-M 2-(4-(2-(4-Chlorobenzamido)ethyl)phenoxy)-2-methylpropanoic acid 2-(4-(2-(4-chlorobenzamido)ethyl)phenoxy)
    2-(4-(2-parachlorobenzamidoethyl)phenoxy)-2-methylpropionic acid 2-(4-{2-[(4-chlorobenzoyl)amino]ethyl}phenoxy)-2-methylpropanoic acid 2-(4-{2-[(4-chlorophenyl)carbonylamino]ethyl}phenoxy)-2-methylpropanoic acid
    2-(4-{2-[(4-chlorophenyl)formamido]ethyl}phenoxy)-2-methylpropanoic acid 2-(p-(2-(p-Chlorobenzamido)ethyl)phenoxy)-2-methylpropionic acid 2-[4-(2-{[(4-chlorophenyl)carbonyl]amino}ethyl)phenoxy]-2-methylpropanoic acid
    2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropanoic acid 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]isobutyric Acid 2-[4-[2-(4-chlorobezamide)ethyl]phenoxy]-2-methylpropanoic acid
    2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl propanoic acid 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl-propanoic acid 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methylpropanoic acid
    2-[P-[2-P-CHLOROBENZAMIDO)ETHYL]PHENOXY]-2-METHYLPROPIONIC ACID 2-{4-[2-(4-chlorobenzamido)ethyl]phenoxy}-2-methylpropanoic acid 41859-67-0
    4CA-0271 859B670 AB00052265
    AB00052265-15 AB00052265_16 AB00052265_17
    AB03023 AB1004588 AC-6817
    AKOS005107743 ANW-42342 API0001705
    AX8116634 Azufibrat B3346
    BCP03700 BCP0726000153 BCP9000398
    BDBM28701 BENAFIBRATE BF
    BF-759 BG0107 BM 15.075
    BM 15075 BM-15.075 BM-15075
    BPBio1_000589 BRD-K46018455-001-06-0 BRD-K46018455-001-17-7
    BRN 4267656 BSPBio_000535 BSPBio_001314
    BSPBio_003119 Befizal Beza-Lande
    Beza-Puren Bezabeta Bezacur
    Bezafibrat Bezafibrat PB Bezafibrate (JP17/USAN/INN)
    Bezafibrate [USAN:BAN:INN:JAN] Bezafibrate [USAN:INN:BAN:JAN] Bezafibrate, >=98%, solid
    Bezafibrate, European Pharmacopoeia (EP) Reference Standard Bezafibrate, analytical reference material Bezafibrate,(S)
    Bezafibrato Bezafibrato [INN-Spanish] Bezafibrato [Spanish]
    Bezafibratum Bezafibratum [INN-Latin] Bezalip
    Bezalip Retard Bezalip SR Bezamerck
    Bezatol Bezatol SR (TN) Bio2_000034
    Bio2_000514 C19H20ClNO4 CAS-41859-67-0
    CCG-39683 CCRIS 9085 CHEBI:47612
    CHEMBL264374 CS-2874 CTK8B3343
    Cedur D01366 DB01393
    DSSTox_CID_9869 DSSTox_GSID_29869 DSSTox_RID_78826
    DTXSID3029869 Difaterol DivK1c_000092
    EINECS 255-567-9 Eulitop FT-0622617
    GTPL2668 HMS1361B16 HMS1569K17
    HMS1791B16 HMS1921H16 HMS1989B16
    HMS2089F04 HMS2092B12 HMS2096K17
    HMS2233E22 HMS3261D21 HMS3369B13
    HMS3402B16 HMS3650K22 HMS3652M22
    HMS3713K17 HMS500E14 HS-0040
    HY-B0637 IDI1_000092 IDI1_033784
    IIBYAHWJQTYFKB-UHFFFAOYSA-N K-8763 KBio1_000092
    KBio2_000034 KBio2_001923 KBio2_002602
    KBio2_004491 KBio2_005170 KBio2_007059
    KBio3_000067 KBio3_000068 KBio3_002619
    KBioGR_000034 KBioGR_000669 KBioSS_000034
    KBioSS_001923 LO 44 LP00500
    LS-124535 Lipox MCULE-9775992840
    MFCD00078970 MLS000028533 MLS001148205
    NCGC00016850-01 NCGC00016850-02 NCGC00016850-03
    NCGC00016850-04 NCGC00016850-05 NCGC00016850-06
    NCGC00016850-07 NCGC00016850-08 NCGC00016850-09
    NCGC00016850-10 NCGC00016850-11 NCGC00016850-12
    NCGC00016850-15 NCGC00023317-03 NCGC00023317-04
    NCGC00023317-05 NCGC00023317-06 NCGC00023317-07
    NCGC00023317-08 NCGC00255376-01 NCGC00261185-01
    NINDS_000092 NSC-758174 NSC758174
    Opera_ID_376 PEM Pharmakon1600-01502046
    Prestwick0_000378 Prestwick1_000378 Prestwick2_000378
    Prestwick3_000378 Prestwick_724 Propanoic acid, 2-(4-(2-((4-chlorobenzoyl)amino)ethyl)phenoxy)-2-methyl-
    Propanoic acid, 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl- Propionic acid, 2-(4-(2-((4-chlorobenzoyl)amino)ethyl)phenoxy)-2-methyl- PubChem4066
    Q577387 Reducterol Regadrin B
    SB17361 SBI-0051715.P002 SC-04393
    SCHEMBL16299 SMR000058298 SPBio_000824
    SPBio_002456 SPECTRUM1502046 SR-01000000106
    SR-01000000106-10 SR-01000000106-3 SR-01000000106-4
    SR-01000000106-5 ST51014927 SW196871-4
    Sklerofibrat Solibay Spectrum2_000922
    Spectrum3_001500 Spectrum4_000325 Spectrum5_001079
    Spectrum5_001967 Spectrum_001443 TR-016482
    Tox21_110645 Tox21_110645_1 Tox21_301845
    Tox21_500500 UNII-Y9449Q51XH VA10400
    W-106291 Y9449Q51XH ZINC3956919
    bezafibrate durabezur s4159

    DrugBank Name Bezafibrate
    DrugBank DB01393
    CAS Number 1189452-53-6, 41859-67-0, 63927-29-7
    PubChem Compound 39042
    KEGG Drug D01366
    PubChem.Substance 46509188
    ChEBI 47612
    PharmGKB PA162364313
    ChemSpider 35728
    BindingDB 28701.0
    TTD DAP001182
    Wikipedia Bezafibrate
    HET PEM
    DPD 949

    1. Chan et al. (2017)